• Title/Summary/Keyword: Intestinal absorption

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Does Agitation Condition Affect the Correlation Between in vitro Permeability of Xenobiotics across Caco-2 Cells and in vivo Bioavailability of the Compounds\ulcorner

  • Yoo, Ho-Jung;Kim, In-Wha;Hong, Soon-Sun;Chung, Suk-Jae;Shim, Chang-Koo
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.419.2-420
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    • 2002
  • Caco-2 is a cell line derived from the human colon adenocarcinoma and often used as a model for studying intestinal drug absorption. It has been well-known that a strong correlation holds between in vitro permeability across Caco-2 cell monolayers and in vivo bioavailability for various drugs. but the correlation curves varied depending on laboratories. The permeabilities of drugs across Caco-2 cell monolayers have been measured under different agitation conditions. (omitted)

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STUDIES ON BIOLOGICALLY ACTIVE SUBSTANCES IN NON-SAPONIN FRACTION OF KOREAN RED GINSENG

  • Okuda Hiromichi;Zheng Yinan;Matsuura Yukinaga;Takaku Takeshi;Kameda Kenji
    • Proceedings of the Ginseng society Conference
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    • 1993.09a
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    • pp.110-112
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    • 1993
  • Acidic polysaccharide from Korean red ginseng was found to inhibit pancreatic lipase activity and cause reduction of plasma triglyceride level after oral administration of corn oil emulsion to rats. Thus acidic polysaccharide may reduce plasma triglyceride through its inhibitory action on pancreatic lipase and successive inhibition of intestinal absorption of fat due to reduction of lipolysis. In the course of this experiment, we found an unknown ninhydrin positive substance in Korean red ginseng. The unknown substance was identified to be arginyl-fructosyl glucose(Arg - Fru - Glc). Coment of this new compound was $5.37\%$ in Korean red ginseng powder. Sucrase and maltase activities in mucous layer of rat jejunum were found to be inhibited by Arg-Fru-Glc. Physiological significance of the new compound was discussed based on these experimental results.

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ACAT Inhibition of Polyactylenes from Gymnaster koraiensis

  • Jung, Hyun-Ju;Hung, Tran-Manh;Na, Min-Kyun;Min, Byung-Sun;Kwon, Byoung-Mog;Bae, Ki-Hwan
    • Natural Product Sciences
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    • v.15 no.2
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    • pp.110-113
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    • 2009
  • Acyl-coenzyme A: cholesterol acyltransferase (ACAT) catalyzes cholesterol esterification and plays important roles in intestinal absorption of cholesterol, hepatic production of lipoproteins and accumulation of cholesteryl ester within macrophages and smooth muscle cells. In our study, eight polyacetylenes (1 - 8), were isolated from the roots of Gymnaster koraiensis, and their chemical structures were identified on the basis of spectroscopic analysis and mass. Compound 2 with the (10S)-15,16-epoxy group in skeleton strongly inhibited ACAT enzyme with $IC_{50}$ value of 35.8 ${\mu}g$/mL, meanwhile the other compounds displayed significant inhibition of ACAT enzyme with the $IC_{50}$ values from 45.5 to 55.1 ${\mu}g$/mL.

Effects of Lipopolysaccharide on Pharmacokinetics of Drugs

  • Yang, Kyung-Hee;Lee, Myung-Gull
    • Toxicological Research
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    • v.23 no.4
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    • pp.289-299
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    • 2007
  • Lipopolysaccharide (LPS) endotoxin is an active component in the outer membrane of Gram-negative bacteria. LPS is usually used as an inflammatory animal model. During the inflammation, diarrhea and changes in plasma proteins, in hepatic and/or intestinal microsomal cytochrome P450 (CYP) isozymes, and in the renal and/or biliary excretion of drugs have been reported. Thus, in rats pretreated with lipopolysaccharide endotoxin isolated from Klebsiella pneumoniae (KPLPS rats), the absorption, distribution, metabolism, and excretion of drugs could be expected to be altered. Interestingly time-dependent effects on the hepatic CYP isozymes have been reported in KPLPS rats. Thus, in KPLPS rats, the pharmacokinetics of drugs which are mainly metabolized via CYP isozymes could be expected to be time-dependent. In this review, an attempt to explain changes in pharmacokinetics of drug reported in the literature was made in terms of CYP isozyme changes or urinary and/or biliary excretion changes in KPLPS rats.

Preventive Mechanisma of ${\beta}$-Glucan on the Experimental Atherosclerosis in Rats (실험적으로 동맥경화증을 유발시킨 랫드에서 ${\beta}$-Glucan의 동맥경화 방어기전에 대한 연구)

  • 김형욱;이영순
    • Biomolecules & Therapeutics
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    • v.1 no.1
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    • pp.109-120
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    • 1993
  • Mechanisms for the hypocholesterolemic effetcs of $\beta$-glucan remain unclear. Rats were divided into 3 groups; normal control group, atherogenic group(oral administration of cholesterol 40 mg/kg/day and vitamin $D_2$320,000 IU/kg/day),${\beta}$-glucan treatment group(oral administration of atherogenic treatment and ${\beta}$-glucan 0.135 g/kg/day). The ${\beta}$-glucan treatment group showed moderate increases of serum lipids concentration compared with atherogenic group. In histopathological examination, aortas showed no critical lesions. The total fecal neutral sterols and bile acids excreted for 6 days was increased compared with both normal and atherogenic group. These result\ulcorner suggest that mechanisms for the hypocholesterolemic effect of ${\beta}$-glucan on rats were due to the inhibition of cholesterol absorption in the intestinal lumen and acceleration of cholesterol catabolism in the liver.

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Pharmaceutical Studies of Cefoperazone Phthalidyl Ester, a Novel Prodrug of Cefoperazone (세포페라존프탈리딜에스텔의 약제학적 연구)

  • Choi, Seung-Ho;Park, Gee-Bae;Choi, Young-Wook;Kim, Johng-Kap
    • Journal of Pharmaceutical Investigation
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    • v.17 no.4
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    • pp.183-188
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    • 1987
  • A new cephalosporin derivative, cefoperazone phthalidyl ester, were synthesized and investigated in terms of dissolution and absorption properties. In comparison with cefoperazone, its phthalidyl ester showed the following characteristics. The mean dissolution time and variance of retention time were more significantly prolonged in simulated intestinal fluid than those in simulated gastric fluid. After a single oral dosing of both cefoperazone and its ester to rabbits, serum concentrations of cefoperazone were measured by bioassay, and the results showed that the ester exhibited much higher and more sustained blood level than the parent drug. The total area under the curve of cefoperazone phthalidyl ester were 10.8 times greater than that of cefoperazone.

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Effects of Transferrin on Enhancing Biological Availability of Iron

  • Park, In-wook;Kim, Yun-Ji;Seong, i-Seung
    • Preventive Nutrition and Food Science
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    • v.3 no.3
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    • pp.248-250
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    • 1998
  • In this study, transferrin which is an iron-carrying glycoprotein in plasma was evaluted for its iron binding capacities(TIBC), iron solubilizing abilities, and enhancing effect of biological availbability of iron. Results of TIBC showed that 1 mg of transferrin could blind 1.28$\mu\textrm{g}$ of iron indicating that one molecule of transferrin can bind about 2 molecules of iron. Also, solubility of iorn (7.5$\mu\textrm{g}$ Fe/ml) was significantly incresed to 96.0% with addition of transferrin (5mg/ml) .When FeCl3(80$\mu\textrm{g}$ Fe/ml) was injected to iron-deficient rats by intestinal segment in situ technique, 18.4% of injected iron was absorbed wherease 48.49 and 48.76% of injected iron was absorbed with addition of 10 and 20 mg transferrin/ml , respectively.

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Measurement of ileal permeability with different-sized polyethylene glycols (PEG 400, 600 and 1000)

  • Kim, Mee-Hye
    • Archives of Pharmacal Research
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    • v.19 no.2
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    • pp.100-105
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    • 1996
  • Polyethylene glycols (PEGs; 400, 600, and 1000) were used to study the molecular weight (MW) permeability dependence in the rat ileal mucosa. Absorption of the PEGs was measured by following their recirculation perfusion over a 3 hr collection period. HPLC methods were used to separate and quantitate the individual oligomers present in the solution of PEGs mixtures (MW range 330 to 1 1 22 D). In the range studied, a distinct molecular weight cutoff was not identified. Corrected for the length of ileum used in the study, over the molecular weight range 330 to 1122 D, the apparent permeability $(P_{app)$ of PEG ranged from $3.2\pm0.06\times10_{-5} cm/sec(mean\pmSEM, n=7)\; to\; 0.1\pm0.02\times10^{-5} cm/sec.$ Also, it was observed that the apparent permeability was inversely proportional to approximately $MW^{2.4}$.

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Prebiotics: An overview of current researches and industrial applications (프리바이오틱스 최신 연구 현황 및 제품 개발 동향)

  • Hwang, Hye Won;Lee, Dong-Woo
    • Food Science and Industry
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    • v.52 no.3
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    • pp.241-260
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    • 2019
  • Prebiotics are defined as substrates that are selectively utilized by host microorganisms conferring various health benefits. Current prebiotic researches not only focus on non-digestible oligosaccharides, but also extend to polyphenols and peptides. However, the extended scope of prebiotic research pertains its original purposes: promotion of beneficial bacteria in host guts and production of valuable metabolites. Maintenance of optimal gut microflora plays a key role in host health care benefits including anti-cancer activity, immune response modulation, blood lipid level reduction, increased mineral absorption, and weight loss. With increasing probiotics markets, prebiotics have also received much attention in functional food markets. Hence, many global food companies tempt to develop new prebiotics applicable for preventing human diseases as well as modulating immune system. In this review, we discuss current status of prebiotics research, market progress, and future perspectives of prebiotics.

A novel role of Hippo-Yap/TAZ signaling pathway in lymphatic vascular development

  • Cha, Boksik;Moon, Sungjin;Kim, Wantae
    • BMB Reports
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    • v.54 no.6
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    • pp.285-294
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    • 2021
  • The lymphatic vasculature plays important role in regulating fluid homeostasis, intestinal lipid absorption, and immune surveillance in humans. Malfunction of lymphatic vasculature leads to several human diseases. Understanding the fundamental mechanism in lymphatic vascular development not only expand our knowledge, but also provide a new therapeutic insight. Recently, Hippo-YAP/TAZ signaling pathway, a key mechanism of organ size and tissue homeostasis, has emerged as a critical player that regulate lymphatic specification, sprouting, and maturation. In this review, we discuss the mechanistic regulation and pathophysiological significant of Hippo pathway in lymphatic vascular development.